Netarsudil Mesylate


Catalog No. size PriceQuantity
M6862-2 2mg solid $210
M6862-10 10mg solid $836

Description

Cas:1253952-02-1 (HCl)

Product Information

Netarsudil, also known as AR-11324, is a Rho-associated protein kinase inhibitor. Netarsudil is potential useful for treating glaucoma and/or reducing intraocular pressure. Netarsudil Increases Outflow Facility in Human Eyes Through Multiple Mechanisms. Netarsudil inhibited kinases ROCK1 and ROCK2 with a Ki of 1 nM each, disrupted actin stress fibers and focal adhesions in TM cells with IC50s of 79 and 16 nM, respectively, and blocked the profibrotic effects of TGF-β2 in HTM cells. Netarsudil produced large reductions in IOP in rabbits and monkeys that were sustained for at least 24 h after once daily dosing, with transient, mild hyperemia observed as the only adverse effect.

 

Chemical Formula: C30H35N3O9S2

 

Exact Mass: 645.18147

 

Molecular Weight: 645.742

 

Elemental Analysis: C, 55.80; H, 5.46; N, 6.51; O, 22.30; S, 9.93

 

Related CAS#:

1422144-42-0 (mesylate)   

1254032-66-0 (free base)   

1253952-02-1 (HCl)    

 

Synonym: 

 

AR-13324

Netarsudil Mesylate

Rhopressa

 

Chemical Name:

(S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate dimethanesulfonate

 

InChi Key: 

QQDRLKRHJOAQDC-FBHGDYMESA-N

 

InChi Code: InChI=1S/C28H27N3O3.2CH4O3S/c1-18-3-10-25(19(2)13-18)28(33)34-17-20-4-6-21(7-5-20)26(15-29)27(32)31-24-9-8-23-16-30-12-11-22(23)14-24;2*1-5(2,3)4/h3-14,16,26H,15,17,29H2,1-2H3,(H,31,32);2*1H3,(H,2,3,4)/t26-;;/m1../s1

 

Smiles Code:

CS(=O)(O)=O.CS(=O)(O)=O.O=C(OCC1=CC=C([C@@H](CN)C(NC2=CC3=C(C=NC=C3)C=C2)=O)C=C1)C4=CC=C(C)C=C4C

Technical Data:

 

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

 

References

 

  1. Ploysangam P, Patel SP. A Case Report Illustrating the Postoperative Course of Descemetorhexis without Endothelial Keratoplasty with Topical Netarsudil Therapy. Case Rep Ophthalmol Med. 2019 Oct 13;2019:6139026. doi: 10.1155/2019/6139026. eCollection 2019. PubMed PMID: 31737390; PubMed Central PMCID: PMC6815562.

 

  1. Mehran NA, Sinha S, Razeghinejad R. New glaucoma medications: latanoprostene bunod, netarsudil, and fixed combination netarsudil-latanoprost. Eye (Lond). 2019 Nov 6. doi: 10.1038/s41433-019-0671-0. [Epub ahead of print] Review. PubMed PMID: 31695162.

 

  1. Sinha S, Lee D, Kolomeyer NN, Myers JS, Razeghinejad R. Fixed combination netarsudil-latanoprost for the treatment of glaucoma and ocular hypertension. Expert Opin Pharmacother. 2019 Oct 30:1-7. doi: 10.1080/14656566.2019.1685499. [Epub ahead of print] PubMed PMID: 31663782.

 

  1. Radell JE, Serle JB. Netarsudil/latanoprost fixed-dose combination for the treatment of open-angle glaucoma or ocular hypertension. Drugs Today (Barc). 2019 Sep;55(9):563-574. doi: 10.1358/dot.2019.55.9.3039670. PubMed PMID: 31584573.

 

  1. Asrani S, Robin AL, Serle JB, Lewis RA, Usner DW, Kopczynski CC, Heah T; MERCURY-1 Study Group. Netarsudil/Latanoprost Fixed-Dose Combination for Elevated Intraocular Pressure: Three-Month Data from a Randomized Phase 3 Trial. Am J Ophthalmol. 2019 Nov;207:248-257. doi: 10.1016/j.ajo.2019.06.016. Epub 2019 Jun 21. PubMed PMID: 31229466.

 

Products are for research use only. Not for human use.

 

Payment & Security

American Express Apple Pay Diners Club Discover Elo Google Pay JCB Mastercard PayPal Shop Pay Venmo Visa

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed